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KR910011265A - Estrogen-Containing Gel Formulations - Google Patents

Estrogen-Containing Gel Formulations Download PDF

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Publication number
KR910011265A
KR910011265A KR1019900021903A KR900021903A KR910011265A KR 910011265 A KR910011265 A KR 910011265A KR 1019900021903 A KR1019900021903 A KR 1019900021903A KR 900021903 A KR900021903 A KR 900021903A KR 910011265 A KR910011265 A KR 910011265A
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South Korea
Prior art keywords
estrogen
component
gel formulation
containing gel
weight
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Granted
Application number
KR1019900021903A
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Korean (ko)
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KR0173309B1 (en
Inventor
히로시 아케미
다카시 기노시타
사브로 오쓰카
요시후미 호사카
구니오 쓰카모토
요시히사 나카노
Original Assignee
야마구치 에이이치
데이코쿠조키세이야쿠 가부시키가이샤
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Publication of KR910011265A publication Critical patent/KR910011265A/en
Application granted granted Critical
Publication of KR0173309B1 publication Critical patent/KR0173309B1/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
    • A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
    • A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
    • A61K9/7061—Polyacrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7076—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising ingredients of undetermined constitution or reaction products thereof, e.g. rosin or other plant resins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens

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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Dermatology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Botany (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)

Abstract

내용 없음No content

Description

에스트로겐-함유 겔 제제Estrogen-Containing Gel Formulations

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음As this is a public information case, the full text was not included.

제1도는 실시예에서 수득한 겔 제제에 대한 워터 테스트의 방출 결과 그래프도이다1 is a graphical representation of the results of a water test release on the gel formulations obtained in the examples.

Claims (11)

기질이 이의 한쪽 표면에 성분(a)에스트로겐, (b)아크릴레이트 중합체 및 (c) 성분 (b)와 혼화성인 액체 성분을 함유하고 성분(b) : 성분(c)의 중량비가 1.0/0.25 내지 1.0/2.0인 조성무를 가교결합시킴으로써 형성된 가교결합 겔 층을 함유함을 특징으로 하는 에스트로겐-함유겔 제제.The substrate contains, on one surface thereof, a liquid component miscible with component (a) estrogen, (b) acrylate polymer and (c) component (b), and the weight ratio of component (b) to component (c) is from 1.0 / 0.25 to An estrogen-containing gel formulation, characterized in that it contains a crosslinked gel layer formed by crosslinking a composition of 1.0 / 2.0. 제1항에 있어서, 성분(b)가 알킬(메트)아크릴 레이트, 비닐 단량체의 측쇄상에 적어도 하나의 질소원자를 함유하는 포화 또는 불포화 헤테로사이클릭 환이 달린 비닐단량체 및 (메트) 아크릴산을 공중합시켜 수득한 아크릴 공중합체인 에스트로겐-함유 겔 제제.The method of claim 1, wherein component (b) is copolymerized with alkyl (meth) acrylate, a vinyl monomer with a saturated or unsaturated heterocyclic ring containing at least one nitrogen atom on the side chain of the vinyl monomer, and (meth) acrylic acid. Estrogen-containing gel formulation which is an acrylic copolymer obtained. 제1항에 있어서, 성분(a)가 에스트라디올인 에스트로겐-함유 겔 제제.The estrogen-containing gel formulation of claim 1, wherein component (a) is estradiol. 제1항에 있어서, 성분(b) : 성분(c)의 중량비가 1.0/0.4 내지 1.0/2.0인 에스트로겐-함유 겔 제제.The estrogen-containing gel formulation of claim 1, wherein the weight ratio of component (b) to component (c) is from 1.0 / 0.4 to 1.0 / 2.0. 제4항에 있어서, 성분(b) : 성분(c)의 중량비가 1.0/0.6 내지 1.0/1.8인 에스트로겐-함유 겔 제제.The estrogen-containing gel formulation according to claim 4, wherein the weight ratio of component (b) to component (c) is 1.0 / 0.6 to 1.0 / 1.8. 제1항에 있어서, 에스트로겐의 함량이 가교결합된 겔 층의 총량을 기준으로 20중량%이하인 에스트로겐-함유겔 제제.The estrogen-containing gel formulation of claim 1, wherein the content of estrogen is 20% by weight or less based on the total amount of the crosslinked gel layer. 제6항에 있어서, 에스트로겐의 함량이 가교결합된 겔 층의 총량을 기준으로 1 내지 10중량%인 에스트로겐-함유겔 제제.The estrogen-containing gel formulation according to claim 6, wherein the content of estrogen is 1 to 10% by weight based on the total amount of the crosslinked gel layer. 제7항에 있어서, 에스트로겐의 함량이 가교결합된 겔 층의 총량을 기준으로 1 내지 8중량%인 에스트로겐-함유 겔 제제.8. The estrogen-containing gel formulation according to claim 7, wherein the content of estrogen is 1 to 8% by weight based on the total amount of the crosslinked gel layer. 제1항에 있어서, 조성물이 삼작용성 이소시아네이트, 금속 알콜레이트 및 티타늄 또는 알루미늄을 아크릴레이트 중합체 100중량부당 0.01 내지 2.0중량부의 양으로 함유하는 금속 킬레이트 화합물 중에서 선택된 가교결합제를 추가로 함유하는 에스트로겐-함유 겔 제제.The estrogen-containing composition of claim 1, wherein the composition further comprises a trifunctional isocyanate, a metal alcoholate and a crosslinking agent selected from metal chelate compounds containing titanium or aluminum in an amount of 0.01 to 2.0 parts by weight per 100 parts by weight of the acrylate polymer. Gel formulation. 제1항에 있어서, 가교결합된 겔 층의 두께가 10 내지 300㎛인 에스트로겐-함유 겔 제제.The estrogen-containing gel formulation of claim 1, wherein the crosslinked gel layer has a thickness of 10 to 300 μm. 제10항에 있어서, 가교결합된 겔 층의 두께가 40 내지 160㎛인 인스트로겐-함유 겔 제제.The instrogen-containing gel formulation of claim 10, wherein the crosslinked gel layer has a thickness of 40 to 160 μm. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019900021903A 1989-12-28 1990-12-27 Estrogen-containing gel formulation Expired - Fee Related KR0173309B1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
JP344639/89 1989-12-28
JP34463989 1989-12-28
JP23738390A JP3273430B2 (en) 1989-12-28 1990-09-06 Estrogen-containing gel preparation
JP237383/90 1990-09-06
JP237383190 1990-09-06

Publications (2)

Publication Number Publication Date
KR910011265A true KR910011265A (en) 1991-08-07
KR0173309B1 KR0173309B1 (en) 1999-02-01

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KR1019900021903A Expired - Fee Related KR0173309B1 (en) 1989-12-28 1990-12-27 Estrogen-containing gel formulation

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US (1) US5242951A (en)
EP (1) EP0435200B1 (en)
JP (1) JP3273430B2 (en)
KR (1) KR0173309B1 (en)
AT (1) ATE124872T1 (en)
CA (1) CA2033113C (en)
DE (1) DE69020875T2 (en)
DK (1) DK0435200T3 (en)
ES (1) ES2075129T3 (en)
GR (1) GR3017650T3 (en)

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Also Published As

Publication number Publication date
DE69020875D1 (en) 1995-08-17
GR3017650T3 (en) 1996-01-31
CA2033113C (en) 1996-09-03
ES2075129T3 (en) 1995-10-01
CA2033113A1 (en) 1991-06-29
JP3273430B2 (en) 2002-04-08
DE69020875T2 (en) 1995-12-14
EP0435200A2 (en) 1991-07-03
EP0435200B1 (en) 1995-07-12
KR0173309B1 (en) 1999-02-01
EP0435200A3 (en) 1991-09-11
US5242951A (en) 1993-09-07
DK0435200T3 (en) 1995-11-20
JPH03220121A (en) 1991-09-27
ATE124872T1 (en) 1995-07-15

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